Search Results - "MATHIASEN, Joanne R"

The Irwin Test and Functional Observational Battery (FOB) for Assessing the Effects of Compounds on Behavior, Physiology, and Safety Pharmacology in Rodents by Mathiasen, Joanne R, Moser, Virginia C

“…The modified Irwin procedure or functional observational battery (FOB) can be used to achieve several goals. New chemical entities (NCEs) can be behaviorally…”
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The Irwin Test and Functional Observational Battery (FOB) for Assessing the Effects of Compounds on Behavior, Physiology, and Safety Pharmacology in Rodents by Mathiasen, Joanne R, Moser, Virginia C

“…The modified Irwin procedure or functional observational battery (FOB) can be used to achieve several goals. New chemical entities (NCEs) can be behaviorally…”
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Correlation between ex vivo receptor occupancy and wake-promoting activity of selective H3 receptor antagonists by Le, Siyuan, Gruner, John A, Mathiasen, Joanne R, Marino, Michael J, Schaffhauser, Hervé

“…The histamine H3 receptor (H3R) modulates the release of neurotransmitters that are involved in vigilance, cognition, and sleep-wake regulation. H3R antagonism…”
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Discovery and Characterization of 6-{4-[3-(R)-2-Methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, Irdabisant): A Potent, Selective Histamine H3 Receptor Inverse Agonist by Hudkins, Robert L, Raddatz, Rita, Tao, Ming, Mathiasen, Joanne R, Aimone, Lisa D, Becknell, Nadine C, Prouty, Catherine P, Knutsen, Lars J. S, Yazdanian, Mehran, Moachon, Gilbert, Ator, Mark A, Mallamo, John P, Marino, Michael J, Bacon, Edward R, Williams, Michael

“…Optimization of a novel series of pyridazin-3-one histamine H3 receptor (H3R) antagonists/inverse agonists identified…”
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Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: Identification of a potent and selective 5-HT6 receptor antagonist showing activity in rat social recognition test by Tripathy, Rabindranath, McHugh, Robert J., Bacon, Edward R., Salvino, Joseph M., Morton, George C., Aimone, Lisa D., Huang, Zeck, Mathiasen, Joanne R., DiCamillo, Amy, Huffman, Mark J., McKenna, Beth A., Kopec, Karla, Lu, Lily D., Qian, Jie, Angeles, Thelma S., Connors, Thomas, Spais, Chrysanthe, Holskin, Beverly, Duzic, Emir, Schaffhauser, Hervé, Rossé, Gerard C.

“…Serotoninergic neurotransmission has been implicated in modulation of learning and memory. It has been demonstrated that 5-hydroxytryptamine6 (5-HT6) receptor…”
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Dimebolin is a 5-HT6 antagonist with acute cognition enhancing activities by SCHAFFHAUSER, Hervé, MATHIASEN, Joanne R, DICAMILLO, Amy, HUFFMAN, Mark J, LU, Lily D, MCKENNA, Beth A, JIE QIAN, MARINO, Michael J

“…Dimebolin (Dimebon), is a non-selective antihistamine approved in Russia for the treatment of allergy. Recently, this drug has been shown to be neuroprotective…”
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Novel object recognition in the rat: a facile assay for cognitive function by Mathiasen, Joanne R, DiCamillo, Amy

“…The rat novel object recognition (NOR) assay is a relatively high-throughput, robust, and sensitive procedure for evaluating compounds for cognition-enhancing…”
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3-(1′-Cyclobutylspiro[4H-1,3-benzodioxine-2,4′-piperidine]-6-yl)-5,5-dimethyl-1,4-dihydropyridazin-6-one (CEP-32215), a new wake-promoting histamine H3 antagonist/inverse agonist by Hudkins, Robert L., Gruner, John A., Raddatz, Rita, Mathiasen, Joanne R., Aimone, Lisa D., Marino, Michael J., Bacon, Edward R., Williams, Michael, Ator, Mark A.

“…CEP-32215 is a new, potent, selective, and orally bioavailable inverse agonist of the histamine H3 receptor (H3R) with drug-like properties. High affinity in…”
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3,4-Diaza-bicyclo[4.1.0]hept-4-en-2-one phenoxypropylamine analogs of irdabisant (CEP-26401) as potent histamine-3 receptor inverse agonists with robust wake-promoting activity by Hudkins, Robert L., Becknell, Nadine C., Lyons, Jacquelyn A., Aimone, Lisa D., Olsen, Mark, Haltiwanger, R. Curtis, Mathiasen, Joanne R., Raddatz, Rita, Gruner, John A.

“…A novel series of 3,4-diaza-bicyclo[4.1.0]hept-4-en-2-ones were designed and synthesized as H3R analogs of irdabisant 6. Separation of the isomers, assignment…”
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Characterization of pharmacological and wake-promoting properties of the dopaminergic stimulant sydnocarb in rats by Gruner, John A, Mathiasen, Joanne R, Flood, Dorothy G, Gasior, Maciej

“…Sydnocarb is a psychomotor stimulant structurally similar to d-amphetamine (D-AMPH) and is used in Russia for the treatment of a variety of neuropsychiatric…”
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Discovery of (1R,6S)-5-[4-(1-cyclobutyl-piperidin-4-yloxy)-phenyl]-3,4-diaza-bicyclo[4.1.0]hept-4-en-2-one (R,S-4a): Histamine H3 receptor inverse agonist demonstrating potent cognitive enhancing and wake promoting activity by Hudkins, Robert L., Josef, Kurt A., Becknell, Nadine C., Aimone, Lisa D., Lyons, Jacquelyn A., Mathiasen, Joanne R., Gruner, John A., Raddatz, Rita

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Substituted phenoxypropyl-(R)-2-methylpyrrolidine aminomethyl ketones as histamine-3 receptor inverse agonists by Zulli, Allison L., Aimone, Lisa D., Mathiasen, Joanne R., Gruner, John A., Raddatz, Rita, Bacon, Edward R., Hudkins, Robert L.

“…Optimization of a series of aminomethyl ketone diamine H3R antagonists to reduce the brain exposure by lowering the pKa, led to molecules with improved…”
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Social recognition assay in the rat by Mathiasen, Joanne R, DiCamillo, Amy

“…Neuropsychiatric disorders encompass a broad patient population in a variety of disease states across all age groups and are often accompanied by deficits in…”
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4-Phenoxypiperidine pyridazin-3-one histamine H3 receptor inverse agonists demonstrating potent and robust wake promoting activity by Hudkins, Robert L., Zulli, Allison L., Dandu, Reddeppa reddy, Tao, Ming, Josef, Kurt A., Aimone, Lisa D., Curtis Haltiwanger, R., Huang, Zeqi, Lyons, Jacquelyn A., Mathiasen, Joanne R., Raddatz, Rita, Gruner, John A.

“…Structure–activity relationships for a series of phenoxypiperidine pyridazin-3-one H3R antagonists/inverse agonists are disclosed. The search for compounds…”
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Mixed-Lineage Kinase 1 and Mixed-Lineage Kinase 3 Subtype-Selective Dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: Optimization, Mixed-Lineage Kinase 1 Crystallography, and Oral in Vivo Activity in 1-Methyl-4-phenyltetrahydropyridine Models by Hudkins, Robert L, Diebold, James L, Tao, Ming, Josef, Kurt A, Park, Chung Ho, Angeles, Thelma S, Aimone, Lisa D, Husten, Jean, Ator, Mark A, Meyer, Sheryl L, Holskin, Beverly P, Durkin, John T, Fedorov, Alexander A, Fedorov, Elena V, Almo, Steven C, Mathiasen, Joanne R, Bozyczko-Coyne, Donna, Saporito, Michael S, Scott, Richard W, Mallamo, John P

“…The optimization of the dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-one R2 and R12 positions led to the identification of the first MLK1 and MLK3…”
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Synthesis and structure–activity relationship of 5-pyridazin-3-one phenoxypiperidines as potent, selective histamine H3 receptor inverse agonists by Tao, Ming, Aimone, Lisa D., Gruner, John A., Mathiasen, Joanne R., Huang, Zeqi, Lyons, Jacquelyn, Raddatz, Rita, Hudkins, Robert L.

“…Optimization of the R2 and R6 positions of (5-{4-[3-(R)-2-methylpyrrolin-1-yl-propoxy]phenyl}-2H-pyridazin-3-one) 2a with constrained phenoxypiperidines led to…”
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Synthesis and evaluation of pyridone-phenoxypropyl-R-2-methylpyrrolidine analogues as histamine H₃ receptor antagonists by Becknell, Nadine C, Lyons, Jacquelyn A, Aimone, Lisa D, Gruner, John A, Mathiasen, Joanne R, Raddatz, Rita, Hudkins, Robert L

“…6-{4-[3-(R)-2-Methylpyrrolidin-1-yl)propoxy]-phenyl}-2H-pyridazin-3-one 6 (Irdabisant; CEP-26401) was recently reported as a potent H₃R antagonist with…”
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4,5-Dihydropyridazin-3-one derivatives as histamine H3 receptor inverse agonists by Hudkins, Robert L., Aimone, Lisa D., Dandu, Reddeppa reddy, Dunn, Derek, Gruner, John A., Huang, Zeqi, Josef, Kurt A., Lyons, Jacquelyn A., Mathiasen, Joanne R., Tao, Ming, Zulli, Allison L., Raddatz, Rita

“…H3R structure–activity relationships for a new class of 4,5-dihydropyridazin-3-one H3R antagonists/inverse agonists are disclosed. Modification of the…”
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Synthesis and evaluation of pyridazinone–phenethylamine derivatives as selective and orally bioavailable histamine H₃ receptor antagonists with robust wake-promoting activity by Dandu, Reddeppa reddy, Gruner, John A, Mathiasen, Joanne R, Aimone, Lisa D, Hostetler, Greg, Benfield, Caitlyn, Bendesky, Robert J, Marcy, Val R, Raddatz, Rita, Hudkins, Robert L

“…A series of pyridazinone–phenethylamine derivatives with moderate to low nanomolar affinity for rat and human H₃R are described. These analogs exhibited…”
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Novel brain penetrant benzofuropiperidine 5-HT6 receptor antagonists by Sundar, Babu G., Bailey, Thomas R., Dunn, Derek D., Bacon, Edward R., Salvino, Joseph M., Morton, George C., Aimone, Lisa D., Zeqi, Huang, Mathiasen, Joanne R., Dicamillo, Amy, Huffman, Mark J., McKenna, Beth A., Kopec, Karla, Lu, Lily D., Brown, Rebecca, Qian, Jie, Angeles, Thelma, Connors, Thomas, Spais, Chrysanthe, Holskin, Beverly, Galinis, Deborah, Duzic, Emir, Schaffhauser, Herve, Rosse, Gerard C.

“…h5-HT6R Ki=4.4nM; h5-HT6R cAMP IC50=9.8nM; estimated rat % F=36; brain/plasma: 2. 7-Arylsulfonyl substituted benzofuropiperidine was discovered as a novel…”
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